What type of antibiotic is cefazolin?

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Last updated: January 11, 2026 • View editorial policy

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What Type of Drug is Cefazolin

Cefazolin is a first-generation cephalosporin antibiotic, which is a semi-synthetic beta-lactam antimicrobial agent administered parenterally. 1

Chemical Classification and Structure

  • Cefazolin belongs to the cephalosporin class of antibiotics, specifically classified as a first-generation cephalosporin. 1, 2
  • It contains a beta-lactam ring structure but has a different molecular configuration than penicillins, with unique R1 side chains that do not match any currently available penicillins. 3, 4
  • The chemical structure is the sodium salt of 3-{[(5-methyl-1,3,4-thiadiazol-2-yl)thio]-methyl}-8-oxo-7-[2-(1H-tetrazol-1-yl) acetamido]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid. 1

Mechanism of Action and Antimicrobial Spectrum

  • Cefazolin is bactericidal against most gram-positive cocci (including methicillin-susceptible Staphylococcus aureus and Streptococcus species) and many gram-negative bacilli of clinical importance. 2, 4
  • It demonstrates greater stability against certain beta-lactamases compared to penicillins, though not all. 4
  • The drug is not active against enterococci, Bacteroides fragilis, or Pseudomonas aeruginosa. 2

Clinical Applications

  • Cefazolin is the antibiotic of choice for surgical prophylaxis in most procedures, as recommended by major surgical societies including the American Society of Health-Systems Pharmacists, Infectious Diseases Society of America, Surgical Infection Society, and Society for Healthcare Epidemiology of America. 5
  • It is specifically recommended for prophylaxis in cardiac surgery, orthopedic surgery, neurosurgery, gastrointestinal procedures, urological procedures, obstetric/gynecologic surgery, and plastic surgery. 5
  • The Australian Therapeutic Guidelines state that cefazolin is preferable for most procedures when prophylaxis is needed. 5

Pharmacokinetic Advantages

  • Cefazolin has a longer half-life than many other beta-lactams, requiring less frequent dosing. 4
  • It achieves high tissue concentrations, including intra-amniotic concentrations, with a tissue penetration ratio of approximately 1.06 (tissue/serum free drug area under the curve). 4, 6
  • Each vial contains 48 mg of sodium per 1 gram of cefazolin sodium. 1

Safety Profile in Penicillin Allergy

  • Cefazolin demonstrates negligible cross-reactivity with penicillins (0.7-0.8%) because it does not share side chains with any currently available penicillins, making it safe for patients with penicillin allergy, including those with immediate-type reactions. 3, 7
  • The Dutch Working Party on Antibiotic Policy (SWAB) provides a strong recommendation with moderate quality evidence that cefazolin can be safely administered to patients with penicillin allergy regardless of severity or timing of the index reaction. 3

References

Research

Cephalosporin antibiotics.

Mayo Clinic proceedings, 1983

Guideline

Cephalosporin Selection for Patients with Penicillin Allergy

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

Guideline

Cefazolina vs Oxacilina: Diferencias y Uso Clínico

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

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